Tyrphostin 9

Catalog No.S2895

Tyrphostin 9 is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.

Price Stock Quantity  
USD 190 In stock
USD 147 In stock
USD 270 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Tyrphostin 9  Chemical Structure

Tyrphostin 9 Chemical Structure
Molecular Weight: 282.38

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Tyrphostin 9 is available in the following compound libraries:

Product Information

  • Compare EGFR Inhibitors
    Compare EGFR Products
  • Research Area
  • Inhibition Profile

Product Description

Biological Activity

Description Tyrphostin 9 is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.
Targets PDGFR [6] EGFR [1]
IC50 0.5 μM 460 μM
In vitro SF 6847 inhibits the replication of herpes simplex virus type 1 (HSV-1) with IC50 of 40 nM. SF 6847 (50 nM) partly reverses sodium orthovanadate induced HSV-1 plaque formation. SF 6847 (< 400 nM) decreases the phosphorylation of viral phosphoproteins in a dose-dependent manner, but the SF 6847 (< 800 nM)-induced reduction of protein synthesis is not dose-dependent. [2] SF 6847 prevents PDGF-induced tyrosine phosphorylation of LRP in caveolae in human fibroblasts suggesting that PDGF-BB-mediated LRP activation requires tyrosine phosphorylation and therefore activation of PDGFR-β. [3] SF 6847 (1 mM) blocks the strain-induced stimulatory effect on DNA synthesis of fetal lung cells. [4] SF 6847 (1 μM) causes increased exon inclusion of MAPT exon 10. SF 6847 does not affect the translation or stability of the two mRNAs. SF 6847 (1.6 μM) increases the inclusion of MAPT exon 10 by 2-fold in SHSY-5Y cells. [5]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Binding assay The cells are solubilized in 1 mL per 2×107 cells of cold solubilization buffer (50 mM Hepes buffer, pH 7.6, 1% Triton X-100, 150 mM NaCl, 5 mM EGTA, 1 mM PMSF, 50 pg/mL aprotinin, 25 mM benzamidine, 5 pg/mL leupeptin, and 10 kg/mL soybean trypsin inhibitor) for 20 min at 4 ℃. After centrifugation at 1×107g for 30 min, the supernatant is loaded onto a WGA-agarose column and shaken for 2 hours at 4 ℃. The unabsorbed material is removed and the resin is washed twice with HTN buffer (50 mM Hepes, pH 7.6, 0.1% Triton X-100, 150 mM NaCl), twice with HTN buffer containing 1 M NaCl, and twice with HTNG buffer (50 mM Hepes, pH 7.6, 0.1% Triton X-100, 150 mM NaCl, and 10% glycerol). The EGF receptor is eluted batchwise with HTNG buffer containing 0.5 M NADG. The eluted material is stored in aliquots at -70℃ and diluted before use with TMTNG buffer (50 mM Tris-Mes buffer, pH 7.6, 0.1% Triton X-100, 150 mM NaCl, 10% glycerol).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Gazit A, et al. J Med Chem, 1989, 32(10), 2344-2352.

[2] Yura Y, et al. Arch Virol, 1995, 140(7), 1181-1194.

view more

Chemical Information

Download Tyrphostin 9 SDF
Molecular Weight (MW) 282.38
Formula

C18H22N2O

CAS No. 10537-47-0
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms SF 6847, RG-50872
Solubility (25°C) * In vitro DMSO 56 mg/mL (198.31 mM)
Ethanol 56 mg/mL (198.31 mM)
Water <1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Propanedinitrile, 2-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related EGFR Products

  • Erlotinib

    Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • Afatinib (BIBW2992) Dimaleate

    Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.

  • Poziotinib (HM781-36B)

    Poziotinib (HM781-36B) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Phase 2.

  • Gefitinib (ZD1839)

    Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.

    Features:A potent EGFR tyrosine kinase inhibitor.

  • Erlotinib HCl (OSI-744)

    Erlotinib HCl (OSI-744) is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • Afatinib (BIBW2992)

    Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM in cell-free assays, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.

  • Osimertinib (AZD9291)

    Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.

  • Lapatinib

    Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.

  • AG-490 (Tyrphostin B42)

    AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.

  • Rociletinib (CO-1686, AVL-301)

    Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2.

Recently Viewed Items

Tags: buy Tyrphostin 9 | Tyrphostin 9 supplier | purchase Tyrphostin 9 | Tyrphostin 9 cost | Tyrphostin 9 manufacturer | order Tyrphostin 9 | Tyrphostin 9 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us